KR860003246A - Method for preparing 2-guanidino-4- (2-methyl-4-imidazolyl) thiazole dibromite - Google Patents

Method for preparing 2-guanidino-4- (2-methyl-4-imidazolyl) thiazole dibromite Download PDF

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Publication number
KR860003246A
KR860003246A KR1019850007444A KR850007444A KR860003246A KR 860003246 A KR860003246 A KR 860003246A KR 1019850007444 A KR1019850007444 A KR 1019850007444A KR 850007444 A KR850007444 A KR 850007444A KR 860003246 A KR860003246 A KR 860003246A
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KR
South Korea
Prior art keywords
methyl
reaction
inert solvent
guanidino
thiazole
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KR1019850007444A
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Korean (ko)
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KR870000278B1 (en
Inventor
2세 버클리 웬델 큐
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윌리엄 데이비스 훈
화이자 인코포레이티드
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Publication of KR860003246A publication Critical patent/KR860003246A/en
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Publication of KR870000278B1 publication Critical patent/KR870000278B1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

내용 없음No content

Description

2-구아니디노-4-(2-메틸-4-이미다졸일)티아졸 이브롬산염의 제조방법Method for preparing 2-guanidino-4- (2-methyl-4-imidazolyl) thiazole dibromite

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (6)

(a) 2-메틸-4-아세틸이미다졸을 30 내지 90℃의 반응-불활성 용매중에서 적어도 1몰 당량의 HBr의 존재하에, 약 1몰 당량의 Br2로 브롬화시키고 ; (b) 생성되는 2-메틸-4-(브로모아세틸)이미다졸의 산성 슬러리 또는 용액을 (a)에서와 동일하거나 상이한 반응-불활성 용매중에서 35 내지 100℃에서 약 1몰당량의 N-아미디노티오우레아와 반응시키고 ; (c) 생성되는 반응 혼합물로 부터 2-구아니디노-4-(2-메틸-4-아미 다졸일)티아졸 이브롬산염을 단리시킴을 특징으로 하는, 2-구아니디노-4-(2-메틸-4-이미다졸일)티아졸 이브롬산염의 제조방법.(a) 2-methyl-4-acetylimidazole is brominated with about 1 molar equivalent of Br 2 in the presence of at least 1 molar equivalent of HBr in a 30-90 ° C. reaction-inert solvent; (b) An acidic slurry or solution of the resulting 2-methyl-4- (bromoacetyl) imidazole is about 1 molar equivalent of N-amid at 35-100 ° C. in the same or different reaction-inert solvent as in (a). React with dinothiourea; (c) 2-guanidino-4- (2), characterized by isolating 2-guanidino-4- (2-methyl-4-amidazolyl) thiazole dibromite from the resulting reaction mixture. -Methyl-4-imidazolyl) thiazole dibromate. 제1항에 있어서, 단계(a)에서는 단지 약 1몰 당량의, HBr이 사용되며, 언급된 단계(a) 및 (b)모두에서의 반응-불활성 용매가 아세트산인 방법.The process of claim 1 wherein only about 1 molar equivalent of HBr is used in step (a) and the reaction-inert solvent in both steps (a) and (b) mentioned is acetic acid. 제1항에서, 언급된 단계(a) 및 (b) 모두에서의 반응-불활성 용매가 진한 수성 HBr이며, 단계(b)에서의 반응-불활성 용매가 에탄올을 더 함유하는 방법.2. The process of claim 1 wherein the reaction-inert solvent in both mentioned steps (a) and (b) is concentrated aqueous HBr and the reaction-inert solvent in step (b) further contains ethanol. 제1항에 있어서, 단계(a)가 40 내지 80℃에서 수행되는 방법.The process of claim 1 wherein step (a) is performed at 40 to 80 ° C. 제1항에 있어서, 단계(b)가 45 내지 90℃에서 수행되는 방법.The process of claim 1 wherein step (b) is performed at 45 to 90 ° C. 제 4항에 있어서, 단계(b)가 45 내지 90℃에서 수행되는 방법.The process of claim 4 wherein step (b) is performed at 45 to 90 ° C. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019850007444A 1984-10-11 1985-10-10 Process for the preparation of 2-guanidino-4-(2-methyl-4-imidazolyl)thiazole dihydrobromide KR870000278B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US06/659,749 US4632993A (en) 1984-10-11 1984-10-11 Process for making 2-guanidino-4-(2-methyl-4-imidazolyl) thiazole dihydrobromide
US659,749 1984-10-11

Publications (2)

Publication Number Publication Date
KR860003246A true KR860003246A (en) 1986-05-21
KR870000278B1 KR870000278B1 (en) 1987-02-23

Family

ID=24646672

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019850007444A KR870000278B1 (en) 1984-10-11 1985-10-10 Process for the preparation of 2-guanidino-4-(2-methyl-4-imidazolyl)thiazole dihydrobromide

Country Status (16)

Country Link
US (1) US4632993A (en)
EP (1) EP0178123A2 (en)
JP (1) JPS6193181A (en)
KR (1) KR870000278B1 (en)
CN (1) CN85107520A (en)
AU (1) AU558249B2 (en)
DD (1) DD238234A5 (en)
DK (1) DK463785A (en)
ES (1) ES8605268A1 (en)
FI (1) FI853949L (en)
GR (1) GR852440B (en)
HU (1) HUT38633A (en)
IL (1) IL76648A0 (en)
NO (1) NO854034L (en)
PL (1) PL255695A1 (en)
PT (1) PT81281B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4997949A (en) * 1986-10-29 1991-03-05 Pfizer Inc. Crystalline 2-(1-pentyl-3-guanidino)-4-(2-methyl-4-imidazolyl) thiazole dihydrochloride trihydrate
WO1990002127A1 (en) * 1988-08-30 1990-03-08 Pfizer Inc. Hemiphosphate hemihydrate of 2-(1-pentyl-3-guanidino-4-imidazolyl)thiazole
EP1951668B1 (en) * 2005-11-16 2010-04-14 F.Hoffmann-La Roche Ag Novel process for the preparation of thoc
EP1956018A1 (en) * 2007-02-06 2008-08-13 Boehringer Ingelheim Pharma GmbH & Co. KG Method of preparing a derivative of benzimidazole
EP4196793A1 (en) 2020-08-11 2023-06-21 Université de Strasbourg H2 blockers targeting liver macrophages for the prevention and treatment of liver disease and cancer

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4374843A (en) * 1980-10-14 1983-02-22 Pfizer Inc. 2-Guanidino-4-heteroarylthiazoles
US4435396A (en) * 1982-05-10 1984-03-06 Pfizer Inc. Antiulcer 2-guanidino-4-(2-substituted-amino-4-imidazolyl)thiazoles and process therefor

Also Published As

Publication number Publication date
US4632993A (en) 1986-12-30
PT81281A (en) 1985-11-01
HUT38633A (en) 1986-06-30
FI853949L (en) 1986-04-12
DK463785A (en) 1986-04-12
ES8605268A1 (en) 1986-03-16
DD238234A5 (en) 1986-08-13
GR852440B (en) 1986-02-10
NO854034L (en) 1986-04-14
PT81281B (en) 1987-08-31
ES547713A0 (en) 1986-03-16
PL255695A1 (en) 1986-07-29
EP0178123A2 (en) 1986-04-16
JPS6193181A (en) 1986-05-12
AU558249B2 (en) 1987-01-22
CN85107520A (en) 1986-07-23
KR870000278B1 (en) 1987-02-23
FI853949A0 (en) 1985-10-10
IL76648A0 (en) 1986-02-28
AU4848785A (en) 1986-04-17
DK463785D0 (en) 1985-10-10

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